Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.11.2.2 extracted from

  • Soubhye, J.; Aldib, I.; Elfving, B.; Gelbcke, M.; Furtmueller, P.G.; Podrecca, M.; Conotte, R.; Colet, J.M.; Rousseau, A.; Reye, F.; Sarakbi, A.; Vanhaeverbeek, M.; Kauffmann, J.M.; Obinger, C.; Neve, J.; Prevost, M.; Zouaoui Boudjeltia, K.; Dufrasne, F.; Van Antwerpen, P.
    Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors (2013), J. Med. Chem., 56, 3943-3958.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-(5-fluoro-1H-indol-3-yl)butanamide reversible myeloperoxidase inhibitor, efficiently prevents enzyme-dependent LDL oxidation Homo sapiens
4-(7-fluoro-1H-indol-3-yl)butanamide
-
Homo sapiens
5-(7-fluoro-1H-indol-3-yl)pentanamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P05164
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
low-density lipoprotein + Cl- + H2O2
-
Homo sapiens ? + H2O enzyme produces oxidative modifications of the protein moiety of low density lipoproteins ?
taurine + Cl- + H2O2
-
Homo sapiens taurine chloramine + H2O
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000018
-
low density lipoprotein oxidation, pH 7.2, 37°C Homo sapiens 4-(5-fluoro-1H-indol-3-yl)butanamide
0.000018
-
taurine chlorination, pH 7.2, 37°C Homo sapiens 4-(5-fluoro-1H-indol-3-yl)butanamide
0.000024
-
low density lipoprotein oxidation, pH 7.2, 37°C Homo sapiens 4-(7-fluoro-1H-indol-3-yl)butanamide
0.000026
-
taurine chlorination, pH 7.2, 37°C Homo sapiens 4-(7-fluoro-1H-indol-3-yl)butanamide
0.000034
-
taurine chlorination, pH 7.2, 37°C Homo sapiens 5-(7-fluoro-1H-indol-3-yl)pentanamide
0.000044
-
low density lipoprotein oxidation, pH 7.2, 37°C Homo sapiens 5-(7-fluoro-1H-indol-3-yl)pentanamide